Journal
CURRENT MEDICINAL CHEMISTRY
Volume 13, Issue 17, Pages 2021-2039Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/092986706777585004
Keywords
Camptothecin; Antitumor; Topo I inhibitor
Funding
- National Science Foundation of China (NSFC)
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The review provides a detailed discussion of recent advances in the medicinal chemistry of camptothecin, a potent antitumor agent that targets topoisomerase I. Thousands of CPT derivatives have been synthesized. Two of them, Topotecan and Irinotecan, are commercially approved for use in clinic as antitumor agents while more are still in clinic trials. This review summarizes the current status of the modern synthetic approaches to CPT, the mechanism of action of CPT, the structure-activity relationship(SAR), a number of novel CPT analogs and their biologic activity. There is a systematic evaluation of A-, B- and E-ring- modified camptothecins reported recently.
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